A patent review of arginine methyltransferase inhibitors (2010-2018)
文献类型：期刊论文
| 作者 | Li, Xiao; Wang, Chen; Jiang, Hao; Luo, Cheng |
| 刊名 | EXPERT OPINION ON THERAPEUTIC PATENTS
 |
| 出版日期 | 2019-02-01 |
| 卷号 | 29期号:2页码:97-114 |
| 关键词 | Arginine methylation Protein arginine methyltransferases (PRMTs) small molecule inhibitors drug research and development |
| ISSN号 | 1354-3776 |
| DOI | 10.1080/13543776.2019.1567711 |
| 通讯作者 | Luo, Cheng(cluo@mail.shcnc.ac.cn) |
| 英文摘要 | Introduction: Protein arginine methyltransferases (PRMTs) are fundamental enzymes that specifically modify the arginine residues of versatile substrates in cells. The aberrant expression and abnormal enzymatic activity of PRMTs are associated with many human diseases, especially cancer. PRMTs are emerging as promising drug targets in both academia and industry. Areas covered: This review summarizes the updated patented inhibitors targeting PRMTs from 2010 to 2018. The authors illustrate the chemical structures, molecular mechanism of action, pharmacological activities as well as the potential clinical application including combination therapy and biomarker-guided therapy. PRMT inhibitors in clinical trials are also highlighted. The authors provide a future perspective for further development of potent and selective PRMT inhibitors. Expert opinion: Although a number of small molecule inhibitors of PRMTs with sufficient potency have been developed, the selectivity of most PRMT inhibitors remains to be improved. Hence, novel approaches such as allosteric regulation need to be further studied to identify PRMT inhibitors. So far, three PRMT inhibitors have entered clinical trials, including PRMT5 inhibitor GSK3326595 and JNJ-64619178 as well as PRMT1 inhibitor GSK3368715. PRMT inhibitors with novel mechanism of action and good drug-like properties may shed new light on drug research and development progress. |
| WOS关键词 | N-METHYLTRANSFERASE ; SUBSTRATE-SPECIFICITY ; PROTEIN METHYLATION ; CRYSTAL-STRUCTURE ; IN-VIVO ; PRMT1 ; IDENTIFICATION ; MEMBER ; FAMILY ; ENZYME |
| 资助项目 | National Natural Science Foundation of China[81625022] ; National Natural Science Foundation of China[91853205] ; National Natural Science Foundation of China[81430084] ; National Natural Science Foundation of China[81821005] ; K. C. Wong Education Foundation ; Chinese Academy of Sciences[XDA12020353] ; Chinese Academy of Sciences[XDA12050401] ; Science and Technology Commission of Shanghai Municipality[18431907100] |
| WOS研究方向 | Pharmacology & Pharmacy |
| 语种 | 英语 |
| WOS记录号 | WOS:000457401800003 |
| 出版者 | TAYLOR & FRANCIS LTD |
| 源URL | [http://119.78.100.183/handle/2S10ELR8/290593]  |
| 专题 | 新药研究国家重点实验室 |
| 通讯作者 | Luo, Cheng |
| 作者单位 | 1.Chinese Acad Sci, Shanghai Inst Mat Med, Drug Discovery & Design Ctr, State Key Lab Drug Res,CAS Key Lab Receptor Res, Shanghai, Peoples R China 2.Univ Chinese Acad Sci, Dept Pharm, Beijing, Peoples R China |
| 推荐引用方式 GB/T 7714 | Li, Xiao,Wang, Chen,Jiang, Hao,et al. A patent review of arginine methyltransferase inhibitors (2010-2018)[J]. EXPERT OPINION ON THERAPEUTIC PATENTS,2019,29(2):97-114. |
| APA | Li, Xiao,Wang, Chen,Jiang, Hao,&Luo, Cheng.(2019).A patent review of arginine methyltransferase inhibitors (2010-2018).EXPERT OPINION ON THERAPEUTIC PATENTS,29(2),97-114. |
| MLA | Li, Xiao,et al."A patent review of arginine methyltransferase inhibitors (2010-2018)".EXPERT OPINION ON THERAPEUTIC PATENTS 29.2(2019):97-114. |
入库方式： OAI收割
来源：上海药物研究所
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